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Recent advances in DNA gyrase-targeted antimicrobial agents
Satish N Dighe1, Trudi A Collet1
1Innovative Medicines Group, Institute of Health & Biomedical Innovation, Queensland University of Technology, 60 Musk Avenue, Kelvin Grove, Qld, 4059, Australia.
European Journal of Medicinal Chemistry
|May 28, 2020
Summary
Antimicrobial resistance is a major global health threat. This review examines DNA gyrase inhibitors, including quinoline and non-quinoline compounds, to combat resistance and improve antibacterial therapies.
Area of Science:
- Microbiology
- Medicinal Chemistry
- Drug Discovery
Background:
- Antimicrobial resistance (AMR) poses a significant global health challenge, causing over 20,000 deaths annually in the US.
- DNA gyrase is a validated antibacterial drug target essential for bacterial DNA replication, repair, and decatenation.
- Fluoroquinolones, a current antibacterial class, target DNA gyrase but face limitations due to rising AMR.
Purpose of the Study:
- To review the structure of DNA gyrase.
- To analyze quinoline and non-quinoline inhibitors of DNA gyrase published between 2015-2019.
- To discuss molecular interactions and structure-activity relationships (SAR) of these inhibitors.
Main Methods:
- Literature review of scientific publications from 2015-2019.
- Analysis of DNA gyrase structures.
- Examination of inhibitor chemical structures and their interactions with DNA gyrase.
- Review of SAR studies.
Main Results:
- Identification and categorization of novel quinoline and non-quinoline DNA gyrase inhibitors.
- Detailed insights into the molecular interactions driving inhibitor efficacy.
- Summary of SAR trends for improved antibacterial drug design.
- Highlighting the structural basis for resistance mechanisms.
Conclusions:
- Understanding DNA gyrase structure and inhibitor interactions is crucial for developing new antibacterials.
- Recent research (2015-2019) offers promising leads for novel inhibitors to overcome AMR.
- SAR studies provide a roadmap for designing next-generation antibiotics targeting DNA gyrase.
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